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Assay Detail

CHEMBL670677

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]raclopride from human Dopamine receptor D2A
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
Linnanen T, Brisander M, Unelius L, Sundholm G, Hacksell U, Johansson AM.
J Med Chem (2000) 43 : 1339 -1349
PubMed 10753471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.76 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281924 1 8.15
CHEMBL26751 1 7.62
CHEMBL280804 1 7.61
CHEMBL417473 1 7.58
CHEMBL281554 1 7.15
CHEMBL281923 1 7.15
CHEMBL27309 1 6.74
CHEMBL285352 1 6.67
CHEMBL281048 1 6.58
CHEMBL26471 1 6.50
CHEMBL27251 1 5.65
CHEMBL282375 1 5.44
CHEMBL27247 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281924 Ki = 7.1 nM 8.15
CHEMBL26751 Ki = 23.8 nM 7.62
CHEMBL280804 Ki = 24.5 nM 7.61
CHEMBL417473 Ki = 26.0 nM 7.58
CHEMBL281554 Ki = 70.8 nM 7.15
CHEMBL281923 Ki = 71.0 nM 7.15
CHEMBL27309 Ki = 182.0 nM 6.74
CHEMBL285352 Ki = 215.0 nM 6.67
CHEMBL281048 Ki = 261.0 nM 6.58
CHEMBL26471 Ki = 317.0 nM 6.50
CHEMBL27251 Ki = 2250.0 nM 5.65
CHEMBL282375 Ki = 3650.0 nM 5.44
CHEMBL27247 Ki = 7980.0 nM 5.10